BAY-678
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
BAY-678 is an orally active, potent and selective inhibitor of human neutrophil elastase (HNE) [1][2].
Human neutrophil elastase (HNE) is a member of the chymotrypsin-like family of serine proteases and is stored in the neutrophil cytoplasm. HNE is a key protease for matrix degradation and high HNE activity is occured in inflammatory diseases. So HNE is a potential target for the treatment of pulmonary diseases such as acute lung injury (ALI), acute respiratory distress syndrome (ARDS), chronic obstructive pulmonary disease (COPD), bronchiectasis (BE), and pulmonary hypertension (PH) [1].
BAY-678 is an orally active, potent and selective inhibitor of human neutrophil elastase (HNE). BAY-678 inhibited HNE reversibly with IC50 value of 20 nM and Ki value of 15 nM. BAY-678 showed no inhibition against 21 related serine proteases, up to a concentration of 30 μM [1].
In rats, BAY-678 showed medium clearance with t1/2 of 1.3h [1].
References:
[1]. von Nussbaum F, Li VM, Allerheiligen S, et al. Freezing the Bioactive Conformation to Boost Potency: The Identification of BAY 85-8501, a Selective and Potent Inhibitor of Human Neutrophil Elastase for Pulmonary Diseases. ChemMedChem. 2015 Jul;10(7):1163-73.
[2]. von Nussbaum F, Li VM, Meibom D, et al. Potent and Selective Human Neutrophil Elastase Inhibitors with Novel Equatorial Ring Topology: in vivo Efficacy of the Polar Pyrimidopyridazine BAY-8040 in a Pulmonary Arterial Hypertension Rat Model. ChemMedChem. 2016 Jan 19;11(2):199-206.
Physical Appearance | A crystalline solid |
Storage | Store at 2-8°C |
M.Wt | 400.4 |
Cas No. | 675103-36-3 |
Formula | C20H15F3N4O2 |
Solubility | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide |
Chemical Name | 5-[(4R)-5-acetyl-1,2,3,4-tetrahydro-6-methyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-4-pyrimidinyl]-2-pyridinecarbonitrile |
SDF | Download SDF |
Canonical SMILES | O=C1N(C2=CC(C(F)(F)F)=CC=C2)C(C)=C(C(C)=O)[C@@H](C3=CN=C(C#N)C=C3)N1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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